Rhenium Diamino Dithiol Complexes. III. Lipophilic Ligands for Endotherapeutic Radiopharmaceuticals
Timothy W. Jackson, Masaharu Kojima and
Richard M. Lambrecht
Australian Journal of Chemistry
53(12) 983 - 987
Published: 2000
Abstract
The chemistry and physical properties of a series of rhenium diamino dithiol (dadt) complexes are described. Liposolubility was enhanced by N-substitution of alkyl chains of C1–C14 length on one ligand structure, with longer chain lengths showing the higher solubility, but with a reduction of radiolabelling yield with 99mTc and 186Re. Among the ReV=O [dadt] complexes synthesized, we found that 2,2,9,9-tetramethyl-4-N-alkyl-4,7-diaza-1,10-decanedithiol (alkyl = C1–C10) resulted in stable and lipiodol-soluble complexes. Biological characteristics of the C6 ligand labelled with 99mTc and 186Re were compared, and indicated that the complexes behaved in a similar manner in rodents. The dadt ligands in combination with 188Re or 186Re and fatty acid oils merit further consideration as endotherapeutic radiopharmaceuticals for treatment of hepatoma and metastatic liver cancer.Keywords: Radiotherapy; rhenium complexes; radiopharmaceuticals; lipophilic ligands.
https://doi.org/10.1071/CH96073
© CSIRO 2000